Development and optimization of alendronate loaded liposomes for oral administration by using response surface methodology


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Article Title: Development and optimization of alendronate loaded liposomes for oral administration by using response surface methodology
Authors: Ailiesei I., Cinteza  O.-L., Orbesteanu A.-M., Cojocaru V., Anuta V.
Affiliation: Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, Bucharest
Physical Chemistry Department, University of Bucharest, Bucharest
Abstract: The aim of this study was to develop an optimal liposomal formulation for bisphosphonic compounds with appropriate in vitro stability and granulometric distribution. Liposomes were obtained by lipid film hydration method and analyzed using DLS and spectrophotometric assays. The Box Behnken design was used to study the influence of individual and combined effects of three factors (phosphatidylcholine: cholesterol ratio, the lipid component: active substance ratio and sonication time) on the responses. The selected dependent variables (responses) were drug encapsulation efficiency (DEE, %) and liposomes size (diameter). The optimum liposome formulation with alendronate was developed using surface response methodology for evaluating the effects of independent variables on the selected responses. The results obtained pointed out that lipid:drug ratio was the predominant factor that influenced drug encapsulation efficiency and liposome size distribution was mainly affected by the lipid:drug ratio and sonication time.
Keywords: liposome formulation, alendronate, design of experiments, oral administration, spectrophotometry
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*Correspondence: Ailiesei Ioana, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, Bucharest, email: chiticioana@yahoo.com